Liquisolid Compacts Technique of Poor Water Soluble Drugs: An Overview

Liquisolid technique is new and promising method that can use to enhance the dissolution rate of poorly water soluble drugs. Liquisolid compact technique is based upon the dissolving the drug in a suitable non-volatile solvent by using carrier and coating material for the conversion of acceptable flowing and compressible powders. By applying the mathematical models the carrier and coating materials optimized. In this case the drug is almost solubilised in the solvent or molecularly dispersed state which contributes the enhanced drug dissolution.

Formulation and Evaluation of Liquisolid Compacts of BCS Class II Drug Ketoprofen

Aims: The main objective of the current research work is to develop liquisolid compacts of BCS Class II drug ketoprofen with an intention to enhance the solubility of drug by applying liquisolid technique. Place and Duration of Study: Smriti College of Pharmaceutical Education between June 2018 June 2019. Methodology: Initially liquid medication was obtained by dissolving drug in suitable solvent. Saturation solubility studies were performed in various hydrophilic non-volatile solvents to select the solvent showing highest solubility for drug. This liquid medication was admixed with calculated amounts of carrier material (Avicel PH 102) and coating material (Cab-O-Sil) using Spireas mathematical model in order to obtain liquisolid formulations. Further, this powder mass of liquisolid system was compressed to form Ketoprofen liquisolid compact formulations ranging from TK1 to TK9. They were further subjected to post compression evaluation tests such as weight variation, hardness, friability, content uniformity, disintegration and in vitro dissolution studies. Results: Based on the solubility studies, PEG 400 was selected as solvent for ketoprofen drug. Rheological properties for the prepared liquisolid powder system were performed for all the formulations and they showed acceptable flow properties. The results obtained for the post compression evaluation tests of all the prepared liquisolid compacts were present within the acceptable limits. The disintegration time observed for all formulations were within 5 minutes. The results of in vitro release of all the liquisolid compacts showed enhanced release rates compared to that of directly compressed tablet. Lquisolid compact formulation TK7 showed maximum release of 97.62% of drug within 12 minutes in pH 7.4 phosphate buffer which was much higher when compared to that of directly compressed tablet. The SEM and PXRD studies for TK7 revealed conversion of crystalline to molecularly dispersed form of drug in the obtained liquisolid formulation. DSC and FTIR studies also revealed that there was no presence of any significant interaction between drug and excipients involved in the formulation. Conclusion: Finally, it could be concluded that Liquisolid technique was successful in enhancing the solubility and further dissolution profile of BCS Class II drug Ketoprofen.

Formulation and Evaluation of Liquisolid Compacts of Zotepine

The aim of present research work is to formulation and evaluates Liquisolid Compacts of Zotepine to improve solubility and dissolution rate of drug. Solubility and dissolution rate of Zotepine was increased by preparing Liquisolid Compacts of Zotepine using PEG as vehicle, Aerosil as coating agent and Avicel as adsorbent and sodium starch glycolate as super disintegrant. FTIR study was checked for possible drug excipient interaction. The hardness of all formulation was found good enough to pass the friability criteria. Hence the friability of the formulation is well within the acceptance criteria. The friability was found less than 1 in all formulations. Further, the drug content of the formulation batches F1-F8 found within acceptance range. The disintegration time of the F1-F8 batches was found less the 60 seconds. It was found that the amount of SSG is directly affecting to DT time of formulation. The F8 formulation was found stable for 1 month during stability study. Liquisolid Compacts of Zotepine were successfully developed by using PEG as vehicle, Aerosil as coating agent and Avicel as adsorbent and sodium starch glycolate as super disintegrant.

Evaluation of the effect of carrier material on modification of release characteristics of poor water soluble drug from liquisolid compacts

Liquisolid compact is a novel dosage form in which a liquid medication (liquid drug, drug solution/dispersion in non-volatile solvent/solvent system) is converted to a dry, free flowing powder and compressed. Objective of the study was to elucidate the effect of carrier material on release characteristics of clopidogrel from liquisolid compacts. Different formulations of liquisolid compacts were developed using microcrystalline cellulose, starch maize, polyvinyl pyrollidone and hydroxypropyl methylcellulose as carrier material in three concentrations (40, 30 and 20%, w/w). Liquid vehicle was selected on the basis of solubility of clopidogrel. Colloidal silicondioxide was used as coating material and ratio of carrier to coating material was kept 10. A control formulation comprised of microcrystalline cellulose (diluents), tabletose-80 (diluents), primojel (disintegrant) and magnesium stearate (lubricant) was prepared by direct compression technique and was used for comparison. All the formulations were evaluated at pre and post compression level. Acid solubility profile showed higher solubility in HCl buffer pH2 (296.89±3.49 μg/mL). Mixture of propylene glycol and water (2:1, v/v) was selected as liquid vehicle. Drug content was in the range of 99–101% of the claimed quantity. All the formulations showed better mechanical strength and their friability was within the official limits (<1%). Microcrystalline cellulose and starch maize resulted in faster drug release while polyvinyl pyrollidone and HPMC resulted in sustaining drug release by gel formation. It is concluded from results that both fast release and sustained release of clopidogrel can be achieved by proper selection of carrier material.

Formulation and evaluation of liquisolid compacts of itraconazole to enhance its oral bioavailability

Aim: Formulate and evaluate liquisolid compacts of Itraconazole, a biopharmaceutical classification system class II drug, which has poor bioavailability. Materials & methods: PEG 600 was used as a nonvolatile solvent, Alfacel PH 200 as a carrier and Aerosil 200 as a coating material. The Itraconazole solution upon mixing with a carrier and coating material resulted in a dry powder, which was compressed into tablets. Results & conclusion: The optimized formulation exhibited a significantly higher drug dissolution (90.73% in 90 min) compared with conventional tablets and marketed capsules. The antifungal activity was retained in the formulation. Higher values of Cmax and AUC0-24 of the formulation compared with the plain drug indicated enhancement in oral bioavailability. The formulation was stable at room temperature as well as in accelerated conditions.